Elacridar (GF120918)

Alias: GW120918; GF-120918; GW 120918; GG-918;GW-0918;GF 120918;GW120918; GW0918; GF120918;GW 0918; GG918; GG 918;
Cat No.:V1296 Purity: ≥98%
Elacridar (formerly GW-120918; GF-120918; GG-918;GW-0918;GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin.
Elacridar (GF120918) Chemical Structure CAS No.: 143664-11-3
Product category: P-gp
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Elacridar (GF120918):

  • Elacridar HCl (GF120918A)
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Elacridar (formerly GW-120918; GF-120918; GG-918; GW-0918; GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin. Elacridar has been used both in vitro and in vivo as a tool inhibitor of P-gp to investigate the role of transporters in the disposition of various test molecules. In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Elacridar (0.001-1 μM; 2 h) reduces the viability of 786-O cells [2]. Elacridar (5 μM; 24 h) modulates P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines [2]. Elacridar (5 μM; 24 h) impacts 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells [2].
ln Vivo
Elacridar (100 mg/kg; intraperitoneally) distributes differently in the brain and plasma[1]. 1.19 Elacridar Plasma Pharmacokinetic Parameters in Mice[1]. AUC0-inf (μg·min/ml) 1460 90.3 161.4 F 0.22 0.013 1 Mice PO 100 mg/kg Mice IP 100 mg/kg Mice IV 2.5 mg/ kg CL/F (ml/min) 2.05 33.2 0.46 Vd/F (liter) 3.5 12.3 0.17 t1/2 (h) 20 4.3 4.4
Cell Assay
Cell Viability Assay[2]
Cell Types: 786-O cells
Tested Concentrations: 2.5 and 5 μM
Incubation Duration: 2 hrs (hours)
Experimental Results: Dose-dependently inhibited cell viability of 786-O cells and demonstrated better inhibitory effect with sunitnib adding Western Blot Analysis[2]
Cell Types: MCF-7, Caki-1, and 786-O cell lines
Tested Concentrations: 5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells.

Cell Viability Assay[2]
Cell Types: MCF-7 and 786-O cell lines
Tested Concentrations: 5 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.
Animal Protocol
Animal/Disease Models: FVB wild-type mice[1].
Doses: 100 mg/kg
Route of Administration: intraperitoneal (ip)injection; 100 mg/kg once
Experimental Results: Showd a higher concertation in brain than plasma except at 4 h after the dose.
References
[1]. Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
[2]. Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C34H33N3O5
Molecular Weight
563.64
CAS #
143664-11-3
SMILES
O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C([H])([H])N(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C1=C([H])C([H])=C([H])C3C(C4C([H])=C([H])C([H])=C(C=4N([H])C=31)OC([H])([H])[H])=O)=O)C([H])([H])C2([H])[H])OC([H])([H])[H]
Synonyms
GW120918; GF-120918; GW 120918; GG-918;GW-0918;GF 120918;GW120918; GW0918; GF120918;GW 0918; GG918; GG 918;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 41 mg/mL (72.7 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
4% DMSO+30% PEG 300+5% Tween 80+ddH2O:1 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7742 mL 8.8709 mL 17.7418 mL
5 mM 0.3548 mL 1.7742 mL 3.5484 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Elacridar (GF120918)A, brain concentrations of topotecan in WT, Mdr1a/b(−/−) (P-gp knockout), Bcrp1(−/−) (Bcrp1 knockout), and Mdr1a/b(−/−)Bcrp1(−/−) (compound P-gp and Bcrp1 knockout) mice at t = 1, 4, 8, 12, and 24 h after dosing. B, brain versus plasma concentration ratios in mice receiving topotecan (single agent; left) and in combination with elacridar (right).Clin Cancer Res.2007 Nov 1;13(21):6440-9.
  • Elacridar (GF120918)

    A, plasma concentration-time profile of topotecan in WT, Mdr1a/b(−/−), Bcrp1(−/−), and Mdr1a/b(−/−)Bcrp1(−/−) mice receiving topotecan as single agent. B, plasma concentration-time profile of topotecan in WT, Mdr1a/b(−/−), Bcrp1(−/−), and Mdr1a/b(−/−)Bcrp1(−/−) mice receiving topotecan in combination with elacridar.Clin Cancer Res.2007 Nov 1;13(21):6440-9.
  • Elacridar (GF120918)

    A, elacridar concentrations in plasma and brain after a single oral dose of 100 mg/kg in FVB wild-type mice. B, brain-to-plasma concentration ratios for elacridar after a single oral dose of 100 mg/kg in FVB wild-type mice.Drug Metab Dispos.2012 Aug;40(8):1612-9.
Contact Us